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Pharmacological evaluation of selected arylpiperazines with atypical antipsychotic potential
Bioorganic & Medicinal Chemistry Letters, 2004 Six active compounds, among previously synthesized and screened arylpiperazines, were selected and evaluated for the binding affinity to rat dopamine, serotonin and alpha(1) receptors. Two compounds with benztriazole group had a 5-HT(2A)/D(2) binding ratio characteristic for atypical neuroleptics (>1, pK(i) values).
Tomić, Mirko +7 more
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Arylpiperazines with Affinity Toward a1-Adrenergic Receptors
Current Medicinal Chemistry, 2002 In the last years, alpha(1) adrenoceptors (alpha(1)-AR) have been the subject of intense research, in part because receptor-binding studies and molecular biology have opened up new aspects of understanding but also because of the potential to find new drugs possibly acting toward pathophysiological processes where alpha(1)-AR are involved, such as ...
MANETTI F. +3 more
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Interaction of Arylpiperazines with the Dopamine Receptor D2 Binding Site [PDF]
Arzneimittelforschung, 2005 The docking of several 1-benzyl-4-arylpiperazines to the dopamine receptor (DAR) D-2 was examined. The results demonstrated that the interaction of protonated NI of the piperazine ring with Asp 86 (III.32) and edge-to-face interactions of the aromatic ...
Vladimir Sukalovic +2 more
exaly +6 more sources
Synthesis of 2‐Benzothienyl Carbonyl 4‐Arylpiperazines as Novel Delavirdine Analogs [PDF]
Synthetic Communications, 2007 A novel series of 2-benzothienyl carbonyl arylpiperazines (6a-f) was synthesized as potential HIV nonnucleoside reverse transcriptase inhibitors (NNRTIs).
Ramiro Araya-Maturana +1 more
exaly +1 more source
European Journal of Medicinal Chemistry, 2016 Arylpiperazines 2–11 were synthesized, and their biological profiles at α1-adrenergic receptors (α1-ARs) assessed by binding assays in CHO cells expressing human cloned subtypes and by functional experiments in isolated rat vas deferens (α1A), spleen ...
Andressa Souza de Oliveira +2 more
exaly +3 more sources
Antimalarials based on the arylpiperazine privileged substructure [PDF]
, 2005 Based on a previous study, arylpiperazines (2-chlorophenylpiperazine, 2-ethoxyphenylpiperazine and phenylpiperazine) were found to be significantly more potent against the chloroquine-resistant (K1) strain than against the chloroquine-sensitive(DIO) strain.
Molyneaux, Carrie-Anne
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Synthesis of Benzo[b]thiophene Carboxamides Connected to 4‐Arylpiperazines through a Benzylic Spacer: Potential Ligands with 5‐HT1A Binding Affinity [PDF]
Synthetic Communications, 2007 New benzothiophene arylpiperazine derivatives 8 (a-f) were synthesized as potential serotoninergic agents with 5-HT1A receptor affinity. Preparation of the derivatives was performed by treating N-[2-(chloromethyl)phenyl]-4,7-dimethoxybenzo[b]thiophene-2 ...
Roberto Acevedo +2 more
exaly +1 more source
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Asymmetric synthesis of 2-arylpiperazines
Bioorganic & Medicinal Chemistry Letters, 2014An asymmetric synthesis of 2-arylpiperazines starting from phenacyl bromides, a variety of which are easily available, has been established. The synthesis features a CBS reduction of phenacyl bromide to provide optically enriched compounds, an SN2 reaction of 1,2,3-oxathiazolidine 2-oxides with an azide anion with invert of configuration, and ...
Satoshi, Yokoshima +4 more
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Molecular Crystals and Liquid Crystals, 2017
Arylpiperazine derivatives referred in this article possessed antitumor activity, which were synthesized and crystallized through the gradual evaporation process.
Zhou, Jinhui +4 more
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Arylpiperazine derivatives referred in this article possessed antitumor activity, which were synthesized and crystallized through the gradual evaporation process.
Zhou, Jinhui +4 more
openaire +2 more sources
Progress in arylpiperazine synthesis by the catalytic amination reaction
Bioorganic & Medicinal Chemistry, 2002Careful base and solvent optimization for catalytic amination is described. A Pd-catalyzed amination between some arylbromide and unprotected piperazine (1equiv) was efficiently carried out with Pd/BINAP catalyst in a toluene-DBU solvent system, which is useful for the one-pot preparation of unsymmetrical piperazine through amination and in-situ N ...
Yasuhiro, Torisawa +2 more
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